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Pinometostat (EPZ5676)

Product #: TS0134
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Details

l  General Information

Product Name

Pinometostat (EPZ5676)

General description

Pinometostat is an S-adenosyl methionine (SAM) competitive inhibitor of protein methyltransferase DOT1L.

Synonym

(2R,3R,4S,5R)-2-(6-aminopurin-9-yl)-5-[[[3-[2-(6-tert-butyl-1H-benzimidazol-2-yl)ethyl]cyclobutyl]-propan-2-ylamino]methyl]oxolane-3,4-diol

Purity

≥98.0%(HPLC)

CAS Number

1380288-87-8

Formula

C30H42N8O3

Molecular Weight

562.71

Suitability

BioReagent, suitable for cell culture, etc.

l  Physical and Chemical Information

Appearance

solid

Solubility(25℃)

DMSO

≥50mg/mL(warmed)

Ethanol

≥50mg/mL(warmed)

Water

Insoluble

l  Biological Information

Biochem/Physiol  Actions

Pinometostat is an S-adenosyl methionine (SAM) competitive inhibitor of protein methyltransferase DOT1L with Ki of 80 pM in a cell-free assay, demonstrating >37,000-fold selectivity against all other PMTs tested, inhibits H3K79 methylation in tumor.

Application

Pinometostat has been used in trials studying the treatment of Leukemia, Acute Leukemias, Acute Myeloid Leukemia, Myelodysplastic Syndrome, and Acute Lymphocytic Leukemia, among others.

l  Storage

Storage temp.

-20℃

l  Precautions and Disclaimer

This product is for R&D use only, not for drug, household, or other uses.

l  References

1.    http://www.drugbank.ca

2.    https://ncit.nci.nih.gov

3.    https://www.ncbi.nlm.nih.gov

 

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